Cancer treatment
AssigneeMorex Development Partners LLP C/O Blue Rock Services
InventorsChristopher Beattie, Anne Wadsworth, James Rennie
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Abstract
A carborane-comprising porphyrin of Formula (1) is provided for use in cancer therapy that extends the period of time between the doses required while the patient is undergoing radiation therapy. The compound can be given not more often than once every 2 or more weeks, avoiding repeated administration, while radiation therapy can continue regularly.
Claims30
A method of treating cancer, comprising administering a compound of the formula (1) as defined below to a patient and repeatedly irradiating the patient, wherein a single dose of the compound is administered not more than once every two weeks:
- wherein:
- R1, R2, R3 and R4 are selected from an electron withdrawing group, —NO2, —NH2, halogen or a substituent represented by the following formula
- wherein Y can be on the ortho, meta or para position on the phenyl rings, and is selected from hydrogen, hydrocarbyl, non-aromatic carbocyclic, non-aromatic heterocyclic, aryl, alkylaryl, arylalkyl;
- or
- a hydrocarbyl, non-aromatic carbocyclic, non-aromatic heterocyclic, aryl, alkylaryl or an arylalkyl group substituted with 1 to 4 hydrophilic groups selected from hydroxy, alkoxy, —C(O)OR5, —SOR6, —SO2R6, nitro, amido, ureido, carbamato, —SR7, —NR8R9 or poly-alkyleneoxide;
- or a substituent represented by formula (3)
- —X—(CR10R11)r—Z (3);
- provided that at least one of R1, R2, R3 and R4 is the substituent represented by formula (2) wherein Y represents formula (3);
- wherein:
- X is selected from oxygen or sulfur;
- R5, R6, R7, R8, R9, R10 and R11 are selected from hydrogen and C1 to C4 hydrocarbyl;
- Z is a carborane cluster comprising at least two carbon atoms and at least three boron atoms, or at least one carbon atom and at least five boron atoms, within a cage structure;
- r is 0 or an integer from 1 to 20;
- a represents an integer from 1 to 4;
- and
- provided also that at least one of R1, R2, R3 and R4 is an electron withdrawing group, —NO2, —NH2 or halogen;
- and
- M is selected from two hydrogen ions, a single monovalent metal ion, two monovalent metal ions, a divalent metal ion, a trivalent metal ion, a tetravalent metal ion, a pentavalent metal ion or a hexavalent metal ion, wherein the porphyrin-metal complex derived from a single monovalent metal ion is charge-balanced by a counter cation, and the porphyrin-metal complex derived from a trivalent, tetravalent, pentavalent or hexavalent metal ion is charge-balanced by an appropriate number of counter anions, dianions or trianions.
Dependencies are inferred from the claim text.